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Synonyms: CFI 400945 | CFI400945
Compound class: Synthetic organic
Comment: CFI-400945 is first-in-class oral, and selective inhibitor of polo-like kinase 4 (PLK4) [1-2]. It has advanced to clinical evaluation in selected cancer patients.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Mason JM, Lin DC, Wei X, Che Y, Yao Y, Kiarash R, Cescon DW, Fletcher GC, Awrey DE, Bray MR et al.. (2014)
Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent.
Cancer Cell, 26 (2): 163-76. [PMID:25043604]
2. Sampson PB, Liu Y, Patel NK, Feher M, Forrest B, Li SW, Edwards L, Laufer R, Lang Y, Ban F et al.. (2015)
The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
J Med Chem, 58 (1): 130-46. [PMID:24867403]
3. Veitch ZW, Cescon DW, Denny T, Yonemoto LM, Fletcher G, Brokx R, Sampson P, Li SW, Pugh TJ, Bruce J et al.. (2019)
Safety and tolerability of CFI-400945, a first-in-class, selective PLK4 inhibitor in advanced solid tumours: a phase 1 dose-escalation trial.
Br J Cancer, 121 (4): 318-324. [PMID:31303643]